69171-85-3Relevant academic research and scientific papers
Linear diarylheptanoids as potential anticancer therapeutics: synthesis, biological evaluation, and structure–activity relationship studies
Motiur Rahman,Lu, Yang,Lee, Hwa-Jong,Jo, Hyunji,Yin, Wencui,Alam, Mohammad Sayed,Cha, Hyochang,Kadi, Adnan A.,Kwon, Youngjoo,Jahng, Yurngdong
, p. 1 - 18 (2018/04/16)
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 -IIα 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 μM, respectively. Among the tested compounds, 7b inhibited topo-I by 9.3% (camptothecin 68.8%), 7e and 7h inhibited topo-IIα by 38.4 and 47.4% (etoposide 76.9%), respectively, at the concentration of 100 μM. 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.
A versatile synthesis of cyclic diphenyl ether-type diarylheptanoids: Acerogenins, (±)-galeon, and (±)-pterocarine
Jeong, Byeong-Seon,Wang, Qian,Son, Jong-Keun,Jahng, Yurngdong
, p. 1338 - 1344 (2008/09/18)
A versatile method for the total synthesis of cyclic diphenyl ether-type diarylheptanoids, acerogenin C, acerogenin L, (±)-galeon, and (±)-pterocarine was described. The Ullmann reaction of suitably substituted linear diphenylheptanoids was employed for t
Mevalonolactone derivatives
-
, (2008/06/13)
This invention concerns novel mevalonolactone derivatives having the formula STR1 wherein A represents a direct linkage, methylene, ethylene, trimethylene or vinylene group; R1 represents hydrogen atom, or an aliphatic acyl group, benzoyl group, or a benzoyl group substituted with hydroxy, lower alkoxy, aliphatic acyloxy or halogen; R2 represents hydrogen atom, a halogen atom or methyl group; and R3, R4 and R5 are same or different and each represents hydrogen atom, a halogen atom, a lower alkyl group with or without halogen as the substituent, phenyl group, or a phenyl group substituted with halogen, lower alkoxy, aliphatic acyloxy or lower alkyl with or without halogen, or a group represented by the formula R6 O-- (in the formula, R6 means hydrogen atom, an aliphatic acyl group, benzoyl group, phenyl group, a phenylalkyl group, cinnamyl group, or a group of benzoyl, phenyl, phenylalkyl or cinnamyl in all of which the aromatic ring is substituted with hydroxy, halogen, lower alkoxy, aliphatic acyloxy or lower alkyl with or without halogen as the substituent, or a lower alkyl group with or without halogen as the substituent). The compounds are useful for the treatment of hyperlipidemia. They may be prepared by halo-lactonizing the corresponding γ,δ-unsaturated carboxylic acid derivatives and optionally dehalogenating the resulting product, or lactonizing the corresponding δ-hydroxy-carboxylic acid derivatives.
