Tag: M.W=200-250

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

A three component protocol has been developed for the synthesis of N-aroyl sulfoximines by the carbonylation of aryl halides followed by nucleophilic attack of NH-sulfoximines. This reaction tolerates a range of aryl iodides and sulfoximines to provide the N-aroyl sulfoximines in good to excellent yields. Less reactive aryl bromides also underwent sulfoximinocarbonylation and afforded the products. This methodol. is free from phosphine ligands. The heterogeneous Pd/C catalyst was successfully recovered and reused for up to five consecutive catalytic cycles.

Sulfoximinocarbonylation of aryl halides using heterogeneous Pd/C catalyst. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

Typical glucose oxidase (GOx)-based starvation therapy is a promising strategy for tumor treatment; however, it is still difficult to achieve an effective therapeutic effect via a single starvation therapy. Herein, we designed a pH-sensitive polymeric vesicle (PV) self-assembled by histamine-modified chondroitin sulfate (CS-his) for codelivery of GOx and L-buthionine sulfoximine (BSO). GOx can consume glucose to induce the starvation therapy after the PVs reach cancer cell. Moreover, the product H2O2 will be reduced by a high concentration of glutathione (GSH) in the tumor cell, resulting in a reduction of the GSH content. The released BSO finally further reduced the GSH level. As a result, the signaling pathway of the ferroptosis will be activated. The in vivo results demonstrated that GOx/BSO@CS PVs exhibit a good inhibitory effect on the growth of 4T1 tumors in mice. Thus, this work provides a facile strategy to prepare pH-sensitive nanomedicine for synergistic starvation-ferroptosis therapy of tumor.

pH-Sensitive Polymeric Vesicles for GOx/BSO Delivery and Synergetic Starvation-Ferroptosis Therapy of Tumor. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

In this study, we have explored the possible role of ascorbic acid (ASC) and glutathione (GSH) in alleviating arsenate (AsV) toxicity in brinjal roots. Moreover, we have also focused our attention on the possible involvement of endogenous nitric oxide (NO) in accomplishing this task. AsV treatment neg. impacts the length and fresh weight of roots and shoots as well as the dry weight and fitness of roots, and this was accompanied by greater As accumulation in roots and shoots of brinjal. AsV treatment also declined the endogenous NO level by inhibiting Nitric Oxide Synthase-like (NOS-like) activity. Furthermore, AsV stimulated oxidative stress markers, caused protein damage by their carbonylation due to downregulation in antioxidants [particularly ascorbate (AsA)-GSH cycle], leading to disturbed cellular redox status. This, collectively, led to root cell death in brinjal. However, the addition of either ASC or GSH rescued brinjal roots from the toxic effects of AsV in. Interestingly, lycorine (an inhibitor of ASC biosynthesis) further increased AsV toxicity, while ASC rescued its effects. Moreover, buthionine sulfoximine (BSO, an inhibitor of GSH biosynthesis) interestingly increased further AsV toxicity, while GSH rescued the plant from the As toxic effects. An interesting notion of this study was that GSH rescued the toxic effect of lycorine, while ASC rescued the toxic effect of BSO, though the AsV toxicity mediated by either ASC or GSH was always accompanied by high endogenous NO level and NOS-like activity. All together, these results suggest that ASC and GSH independently mitigate AsV toxicity in brinjal roots, but both might be dependent on endogenous NO for accomplishing the AsV toxicity alleviatory tasks.

Ascorbate and glutathione independently alleviate arsenate toxicity in brinjal but both require endogenous nitric oxide. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

Volatile oil from traditional Chinese medicine has various biol. activities and has pharmacol. activities in the central nervous system, digestive system, cardiovascular system, respiratory system, etc. These oils are widely used in clin. practice. However, the development of their clin. applications is restricted due to the disadvantages of volatile oils, such as high stimulation, high volatility and poor stability. To improve the stability of a volatile oil in the preparation process, its volatilization and stable release must be controlled. In this paper, porous starch was used as a solid carrier material, and liquid volatile oil was solidified by phys. adsorption. GC-MS was used to determine the chem. constituents of the volatile oil, solidified powder and tablets, and the volatilization rules of 34 chem. constituents were analyzed statistically. The solidified volatile oil/porous starch powder was characterized by XRD, TGA and DSC, and the VOCs of the volatile oil before and after solidification were analyzed by portable GC-MS. Finally, the stable release of the volatile oil could be optimized by changing the porous starch ratio in the formulation. Volatilization was shown to be closely related to the peak retention time and chem. composition, which was consistent with the theory of flavor. The phys. properties and chem. composition of the volatile oil did not change after curing, indicating that the adsorption of the volatile oil by porous starch was phys. adsorption. In this paper, the porous starch-solidified volatile oil had a slow-release effect, and the production process is simple, easy to operate, and has high application value.

Study of the volatilization rules of volatile oil and the sustained-release effect of volatile oil solidified by porous starch. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

A facile protocol for direct oxidative C-N bond coupling of unactivated imidazo[1,2-a]pyridines with NH-sulfoximines was disclosed using sulfoximines as the nitrogen sources in the presence of (diacetoxy)iodobenzene (PhI(OAc)2). The reaction proceeded smoothly under air without any metal catalyst to give a series of C-3 sulfoximidoyl-functionalized imidazo[1,2-a]pyridines products regioselectively.

PhI(OAc)2-mediated oxidative C-H sulfoximination of imidazopyridines under mild conditions. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

N-Arylation of sulfoximines with aryldiazonium tetrafluoroborates was demonstrated in the presence of copper chloride and DABCO. A wide range of aryl and alkyl sufoximines were participated in the coupling reaction with different aryldiazonim salts bearing electron donating and withdrawing groups and provided the desired products in 67-88% yields. The reaction proceeded through a radical mechanism.

Copper catalyzed N-arylation of sulfoximines with aryldiazonium salts in the presence of DABCO under mild conditions. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

A series of desired 2-oxo-2-arylacetyl sulfoximines RC(O)C(O)N=S(O)R1R2 [R = C(CH3)3, 3,4-Cl2C6H3, thiophen-2-yl, naphth-2-yl, etc.; R1 = Me, Et, i-Pr, Ph; R2 = C6H5, 2-ClC6H4, 4-H3COC6H4, etc.; R1R2 = -(CH2)4-] were successfully synthesized in good to excellent yields (up to 93%) under solvent-free conditions using aryl ethanones RC(O)CH3 and NH-sulfoximines R1R2S(O)=NH. The unprecedented protocol requires no extra solvents, bases, or additives and demonstrates outstanding compatibility with assorted functional groups (up to 27 examples). A plausible double catalytic cycle mechanism involving elemental iodine and copper is proposed; in-situ generated aryl-¦Á-iodo-ethanone and a sulfoximine-liganded-CuII intermediate play important roles in C(sp3)-N coupling. The postulated mechanism is inspired by key exptl. investigations detailed here.

CuI-Mediated ¦Á-Ketoacylation of Sulfoximines under Solvent-Free Conditions. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

Abstract: Sorafenib is the first-line treatment of advanced hepatocellular carcinoma (HCC). However, there is a lack of validated biomarkers to predict sorafenib sensitivity. In this study we investigated the role of ACSL4, a pos.-activating enzyme of ferroptosis, in sorafenib-induced cell death and HCC patient outcome. We showed that ACSL4 protein expression was neg. associated with IC50 values of sorafenib in a panel of HCC cell lines (R = -0.952, P < 0.001). Knockdown of ACSL4 expression by specific siRNA/sgRNA significantly attenuated sorafenib-induced lipid peroxidation and ferroptosis in Huh7 cells, and also rescued sorafenib-induced inhibition of xenograft tumor growth in vivo. We selected 29 HCC patients with surgery as primary treatment and sorafenib as postoperative adjunct therapy from a hospital-based cohort. A high proportion (66.7%) of HCC patients who had complete or partial responses to sorafenib treatment (according to the revised RECIST guideline) had higher ACSL4 expression in the pretreated HCC tissues, compared with those who had stable or progressed tumor growth (23.5%, P = 0.029). Since ACSL4 expression was independent of sorafenib treatment, it could serve as a useful predictive biomarker. Taken together, this study demonstrates that ACSL4 is essential for sorafenib-induced ferroptosis and useful for predicting sorafenib sensitivity in HCC. This study may have important translational impacts in precise treatment of HCC. ACSL4 is a predictive biomarker of sorafenib sensitivity in hepatocellular carcinoma. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

Rhodium-catalyzed directed carbene insertions into aromatic C-H bonds of S-aryl sulfoximines led to intermediates, which upon dehydration provided 1,2-benzothiazines, e.g., I, in excellent yields. The domino-type process is regioselective and shows a high functional-group tolerance. It is scalable, and the only byproducts are dinitrogen and water.

Regioselective Syntheses of 1,2-Benzothiazines by Rhodium-Catalyzed Annulation Reactions. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

A copper-catalyzed cross-dehydrogenative C-H/N-H coupling has been devised to access a series of N-arylated sulfoximines, e,g., I, in high yield from 8-aminoquinoline-derived benzamides and sulfoximines. The reaction is scalable, and mechanistic studies favor the involvement of an organometallic pathway, where C-H bond cleavage is presumed to be the kinetically relevant step. The utility of sulfoximine-coupled benzamides was displayed through the nickel-catalyzed acceptorless dehydrogenative olefination of benzyl alcs.

Copper-Catalyzed 8-Aminoquinoline-Directed Oxidative C-H/N-H Coupling for N-Arylation of Sulfoximines. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem