Synthesis, Crystal Structure, and Antiproliferative Activity of Novel 7-Arylaminopyrazolo[1,5-a]pyrimidine Derivatives Containing the Hydrazone Moiety
- Авторы: Shi J.1, Chen Y.1, Ji S.2, Ding S.1, Liu J.1
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Учреждения:
- Key Laboratory of New Drug Research and Development of Liaoning Province
- Jilin Yimintang Pharmaceutical Co., LTD
- Выпуск: Том 89, № 11 (2019)
- Страницы: 2321-2327
- Раздел: Article
- URL: https://journals.rcsi.science/1070-3632/article/view/223180
- DOI: https://doi.org/10.1134/S1070363219110252
- ID: 223180
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Аннотация
A series of novel 7-arylaminopyrazolo[1,5-a]pyrimidine derivatives containing the hydrazone moiety has been synthesized by a five-step procedure including cyclization, chlorination, animation, hydrazinolysis, and condensation. Structures of the products have been characterized by IR, 1H NMR and MS spectra, and single-crystal X-ray diffraction. The bioassay results indicate most of the compounds as potentially antiproliferation agents against A549 and HT-29 cell lines. Among those, compounds 6e and 6f exhibit remarkable inhibitory activity against HT-29 cell lines, that are comparable with that of the positive control sorafenib. Preliminary structure-activity relationship is considered.
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Jian-tao Shi
Key Laboratory of New Drug Research and Development of Liaoning Province
Email: liuju1216@126.com
Китай, Shenyang, Liaoning, 110036
Ye Chen
Key Laboratory of New Drug Research and Development of Liaoning Province
Email: liuju1216@126.com
Китай, Shenyang, Liaoning, 110036
Shengjun Ji
Jilin Yimintang Pharmaceutical Co., LTD
Email: liuju1216@126.com
Китай, Siping, Jilin, 136000
Shi Ding
Key Laboratory of New Drug Research and Development of Liaoning Province
Email: liuju1216@126.com
Китай, Shenyang, Liaoning, 110036
Ju Liu
Key Laboratory of New Drug Research and Development of Liaoning Province
Автор, ответственный за переписку.
Email: liuju1216@126.com
Китай, Shenyang, Liaoning, 110036