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Neo-Tanshinlactone Inspired Synthesis, in vitro Evaluation of Novel Substituted Benzocoumarin Derivatives as Potent anti-Breast Cancer Agents. -A small library of novel benzocoumarin derivatives based on the naturally occurring neo-tanshinlactone scaffold is constructed and their antiproliferative properties against breast cancer cells MCF-7 and MDA-MB-231 are evaluated. A number of derivatives, cf. (I), shows good anti-breast cancer activity, in some cases higher than reference drug tamoxifen. The substances are capable of inducing nuclear fragmentation, cell cycle arrest, and caspase dependent apoptosis in MCF-7 cell lines. In addition, these derivatives are devoid of cytotoxic effect against normal osteoblast cells. -(SASHIDHARA*, K. V.; ROSAIAH, J. N.; KUMAR, M.; GARA, R. K.; NAYAK, L.; SRIVASTAVA, K.; BID, H. K.; KONWAR, R.; Bioorg. Med. Chem. Lett. 20 (2010) 23, 7127-7131, http://dx.doi.org/10.