키다마이드

키다마이드 C화학적 특성, 용도, 생산

개요

Chidamide (Epidaza®), a class I HDAC inhibitor, was discovered and developed by ChipScreen and approved by the CFDA in December 2014 for the treatment of recurrent of refractory peripheral T-cell lymphoma. Chidamide, also known as CS055 and HBI- 8000, is an orally bioavailable benzamide type inhibitor of HDAC isoenzymes class I 1–3, as well as class IIb 10, with potential antineoplastic activity. It selectively binds to and inhibits HDAC, leading to an increase in acetylation levels of histone protein H3.74 This agent also inhibits the expression of signaling kinases in the PI3K/ Akt and MAPK/Ras pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. Currently, phases I and II clinical trials are underway for the treatment of non-small cell lung cancer and for the treatment of breast cancer, respectively.

용도

De-5-fluoro 4-Fluorochidamide is an analogue of Chidamide (CAS 743420-02-0), a hitsone deacetylase inhibitor (HDACI) that enhances gemcitabine (G305000) cytotoxicity in pancreatic cancer cells.

Synthesis

The scalable synthetic approach to chidamide very closely follows the discovery route. The sequence began with the condensation of commercial nicotinaldehyde (52) and malonic acid (53) in a mixture of pyridine and piperidine. Next, activation of acid 54 with N,N0-carbonyldiimidazole (CDI) and subsequent reaction with 4-aminomethyl benzoic acid (55) under basic conditions afforded amide 56 in 82% yield. Finally, activation of 56 with CDI prior to treatment with 4-fluorobenzene- 1,2-diamine (57) and subsequent treatment with TFA and THF yielded chidamide (VIII) in 38% overall yield from 52. However, no publication reported that mono-N-Boc-protected bis-aniline was used to approach Chidamide.

키다마이드 준비 용품 및 원자재

원자재

준비 용품

키다마이드 공급 업체

공급자	전화	이메일	국가	제품 수	이점
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32686	60
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
WinWin Chemical CO., Limited	+86-0577-64498589 +8615325081899	sales@win-winchemical.com	China	14145	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	27945	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
Coresyn Pharmatech Co., Ltd.	+86-571-86626709 +86-18157142896	cbc@coresyn.com	China	9991	58
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3136	58
ShenZhen Trendseen Biological Technology Co.,Ltd.	13417589054	trendseenbio@gmail.com	China	11681	58

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