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Relevant academic research and scientific papers

Isolation, structure elucidation, and syntheses of isoneocryptotanshinone II and tanshinlactone a from Salvia miltiorrhiza

Two new components, isoneocryptotanshinone II (1) and tanshinlactone A (2), were isolated from an EtOH extract of Salvia miltiorrhiza. The structures of 1 and 2 were established by spectroscopic methods and total syntheses. Compound (2) exhibited moderate cytotoxic activities with a CD50 range of 6.87-8.85 μg/mL against the HeLa (cervical epitheloid carcinoma), HepG2 (hepatocellular carcinoma) and OVCAR-3 (ovarian adenocarcinoma) cell lines.

Antitumor agents. 254. Synthesis and biological evaluation of novel neo-tanshinlactone analogues as potent anti-breast cancer agents

In our previous study, neo-tanshinlactone (1) showed potent and selective anti-breast cancer activity. To explore the SAR of 1, nine analogues (15-18, 24-28) were designed and synthesized. Together with 1 and tamoxifen (TAM), all newly synthesized compounds and some intermediates were evaluated for in vitro anticancer activity against several human tumor cell lines. Compounds without a ring D did not show promising activity, while compounds with a methylated furan ring D showed better activity than those with unsubstituted furan or hydroxy-dihydrofuran rings. Among all newly synthesized compounds, compound 15 with an ethyl group at the 4-position showed the best activity and selectivity with ED50 values of 0.45 and 0.18 μg/mL against MCF-7 and ZR-75-1 (ER+) and 13.5 and 10.0 μg/mL against MDA MB-231 and HS 587-1 (ER-), respectively. Furthermore, 15 also showed potent activity against SK-BR-3 (ER-, HER2+) with an ED50 value of 0.10 μg/mL. Our preliminary SAR studies showed that a methylated furan ring D and the C-4 substituent in ring A are critical for anti-breast cancer activity. Further development of 1 and 15 as anti-breast cancer drug candidates is warranted.

NEO-TANSHINLACTONE AND ANALOGS AS POTENT AND SELECTIVE ANTI-BREAST CANCER AGENTS

Compounds of Formulae (I-II) are described : along with methods of using such compounds for the treatment of cancer and pharmeutical formulations thereof.

Antitumor agents. 239. Isolation, structure elucidation, total synthesis, and anti-breast cancer activity of neo-tanshinlactone from Salvia miltiorrhiza

Neo-tanshinlactone (1) was isolated and synthesized for the first time and evaluated in vitro against several human cancer cell lines. Compound 1 showed significant inhibition against two ER+ human breast cancer cell lines and was 10-fold more potent and 20-fold more selective as compared to tamoxifen citrate. Compound 1 also potently inhibited an ER-, HER-2 overexpressing breast cancer cell line. Therefore, this novel compound merits further development as an anti-breast cancer drug candidate.