571188-59-5Relevant articles and documents
Copper-catalyzed selective C-N bond formation with 2-amino, 2-hydroxy and 2-bromo-5-halopyridine
Roy, Swarnali,Paul, Barnali,Mukherjee, Ayan,Kundu, Biswajit,Talukdar, Arindam
, p. 44366 - 44370 (2017)
A copper-catalyzed 1,2-diol amination at the electron-rich C-5 position of unprotected 2-amino/2-hydroxy-5-halopyridine provided excellent yields. Selective amination preferably at C-5 in 2-bromo-5-iodopyridine was achieved under the same conditions. The selective, generally mild and economical coupling reaction at C-5 position described herein could be achieved with amines, heterocycles and amides.
Discovery of novel and orally bioavailable CDK 4/6 inhibitors with high kinome selectivity, low toxicity and long-acting stability for the treatment of multiple myeloma
Yuan, Kai,Kuang, Wenbin,Chen, Weijiao,Ji, Minghui,Min, Wenjian,Zhu, Yasheng,Hou, Yi,Wang, Xiao,Li, Jiaxing,Wang, Liping,Yang, Peng
supporting information, (2021/12/09)
Multiple myeloma (MM) ranks second in malignant hematopoietic cancers, and the most common anti-MM drugs easily generate resistance. CDK4/6 have been validated to play determinant roles in MM, but no remarkable progress has been obtained from clinical trials of CDK4/6 inhibitors for MM. To discover novel CDK6 inhibitors with better potency and high druggability, structure-based virtual screening was conducted to identify compound 10. Further chemical optimization afforded a better derivative, compound 32, which exhibited strong inhibition of CDK4/6 and showed high selectivity over 360+ kinases, including homologous CDKs. The in vivo evaluation demonstrated that compound 32 possessed low toxicity (LD50 > 10,000 mg/kg), favorable bioavailability (F% = 51%), high metabolic stability (t1/2 > 24 h) and strong anti-MM potency. In summary, we discovered a novel CDK4/6 inhibitor bearing favorable drug-like properties and offered a great candidate for MM preclinical studies.
DERIVATIVES OF 4-(IMIDAZO[L,2-A]PYRIDIN-3-YL)-N-(PYRIDINYL)PYRIMIDIN- 2-AMINE AS THERAPEUTIC AGENTS
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Paragraph 0083; 0089; 00137, (2021/01/29)
A novel class of heteroaryl compounds for use in the prevention and/or treatment of proliferative diseases and conditions including cancers. The compounds are considered to be capable of inhibiting cell proliferation by inhibiting the activity of FLT3 and its mutant forms and/or other protein kinases such as CDKs. The compounds have the general structure I:
Anti-cancer quinoxaline pyrimidinamine heterocyclic compound as well as preparation method and application thereof
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Paragraph 0108-0109, (2021/07/21)
The invention discloses an anti-cancer quinoxaline pyrimidinamine heterocyclic compound and a preparation method and application thereof, the structure of the compound is shown as a formula (S), and X is selected from C (O) or (CH2) n; n is 0 or 1; R1 is selected from hydrogen and C1-C8 alkyl; R2 is selected from hydrogen, C1-C8 alkyl, morpholine ring or-NR5R6, and R5 and R6 are selected from hydrogen and C1-C8 alkyl; R3 is selected from hydrogen, methoxyl and halogen; and R4 is selected from hydrogen, C1-C8 alkyl,-S (O) 2Me and-C (O) OC1-C3. The invention also discloses a preparation method and application of the compound.