Linear diarylheptanoids as potential anticancer therapeutics: synthesis, biological evaluation, and structure-activity relationship studies
- 주제(키워드) Linear diarylheptanoids , Topoisomerase-I , Topoisomerase-II , Antiproliferative activity
- 주제(기타) Chemistry, Medicinal; Pharmacology & Pharmacy
- 설명문(일반) [Rahman, A. F. M. Motiur; Yin, Wencui; Kadi, Adnan A.] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia; [Lu, Yang; Cha, Hyochang; Jahng, Yurngdong] Yeungnam Univ, Coll Pharm, Gyongsan 38541, South Korea; [Lee, Hwa-Jong; Jo, Hyunji; Kwon, Youngjoo] Ewha Womans Univ, Coll Pharm, Seoul 03760, South Korea; [Alam, Mohammad Sayed] Jagannath Univ, Dept Chem, Dhaka 1100, Bangladesh
- 등재 SCIE, SCOPUS, KCI등재
- 발행기관 PHARMACEUTICAL SOC KOREA
- 발행년도 2018
- URI http://www.dcollection.net/handler/ewha/000000156168
- 본문언어 영어
- Published As http://dx.doi.org/10.1007/s12272-018-1004-8
- 저작권 이화여자대학교 논문은 저작권에 의해 보호받습니다.
초록/요약
In efforts to develop effective anticancer therapeutics with greater selectivity toward cancerous cell and reduced side-effects, such as emetic effects due to detrimental action of the drug toward the intestinal flora, a series of linear diarylheptanoids (LDHs) were designed and synthesized in 7 steps with good-to-moderate yields. All synthesized compounds were evaluated for their antibacterial, antiproliferative, and topoisomerase-I and -II inhibitory activity. Overall, all compounds showed little to no activity against the bacterial strains tested. Most of the synthesized compounds showed good antiproliferative activity against human breast cancer cell lines (T47D); specifically, the IC50 values of compounds 6a, 6d, 7j, and 7e were 0.09, 0.64, 0.67, and 0.99 M, respectively. Among the tested compounds, 7b inhibited topo-I by 9.3% (camptothecin 68.8%), 7e and 7h inhibited topo-II by 38.4 and 47.4% (etoposide 76.9%), respectively, at the concentration of 100M. These results suggest that a set of promising anticancer agents can be obtained by reducing inhibitory actions on different microbes to provide enhanced selectivity against cancerous cells.
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