868-59-7Relevant articles and documents
Benzo thiazole carboxamides and application thereof
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Paragraph 0034; 0035; 0036, (2019/06/28)
The invention belongs to the technical field of medicines and relates to a benzothiazole formamide compound and application thereof. The benzothiazole formamide compound comprises a derivative of the benzothiazole formamide compound and pharmaceutically applicable salt; a general molecular formula is shown in the description, wherein R1, R2 and Ar are described as claims and the description. The benzothiazole formamide compound and addition salt of the pharmaceutically applicable acid of the compound can be combined with an existing medicine or can be independently utilized as an epidermal growth factor tyrosine kinase inhibitor for treating related diseases of epidermal growth factor acceptor signal transduction disorder, such as small cell lung cancer, squamous cancer, glandular cancer, large cell lung cancer, colorectal cancer, breast cancer, ovarian cancer and renal cell carcinoma. A formula is shown in the description.
Design, synthesis and cytotoxic evaluation of a novel series of benzo[d]thiazole-2-carboxamide derivatives as potential EGFR inhibitors
Zhang, Lan,Deng, Xin-Shan,Zhang, Chao,Meng, Guang-Peng,Wu, Jiao-Feng,Li, Xue-Song,Zhao, Qing-Chun,Hu, Chun
, p. 2180 - 2189 (2017/08/03)
A novel series of benzo[d]thiazole-2-carboxamide derivatives have been de novo designed based on virtual screening methods. The target compounds were synthesized and evaluated for the cytotoxicity against epidermal growth factor receptor high-expressed cancer cell lines (A549, HeLa, and SW480), epidermal growth factor receptor low-expressed cell line (HepG2) and human liver normal cell line (HL7702). Several target compounds have showed moderate to excellent potency against A549, HeLa, and SW480 and weak cytotoxic effects against HepG2, which implies they are probably epidermal growth factor receptor inhibitors. And scarcely did they exhibit any activities against HL7702, which signifies they are likely to overcome the nonspecific toxicity against normal cells. Especially, the compound 6-[2-(diethylamino)-2-oxoethoxy]-N-(furan-2-ylmethyl)benzo[d]thiazole-2-carboxamide (6i) was identified as a promising agent, exhibiting the most potent cytotoxic activities with IC50 values of 4.05, 12.17, 6.76 μM against the A549, HeLa, and SW480 cell lines, respectively.
Novel thiazolidine derivatives as chiral catalysts in the enantioselective addition of diethylzinc to aldehydes
Meng, Qinglin,Li, Yuelan,He, Yan,Guan, Yedi
, p. 4255 - 4261 (2007/10/03)
New chiral thiazolidine derivatives were synthesized conveniently from natural L-cysteine and showed good enantioselectivity (up to 90% ee) in the addition of diethylzinc to aldehydes. The catalytic efficiency of the thiazolidine derivatives is influenced by the different structures of the thiazolidine rings and the bulkiness of R moiety in the ester groups. (C) 2000 Elsevier Science Ltd.
Sulfur-containing β-amino alcohols as catalysts in enantioselective synthesis
Trentmann, Wilhelm,Mehler, Thomas,Martens, Juergen
, p. 2033 - 2043 (2007/10/03)
Oxazaborolidine catalysts generated in situ from cyclic or acyclic sulfur containing (R)-cysteine, (S)-penicillamine and (S)-methionine derivates and BH3 have been applied successfully to the enantiocontrolled, catalytic reduction of aromatic ketones. The corresponding sec alcohols could be obtained in excellent enantiomeric excess, up to 100% ee. Using these chiral auxiliaries in the enantioselective addition of diethylzinc to aldehydes afforded optically active sec alcohols in enantiomeric excess up to 93% ee.
