p388/adr

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.

Dihydrocytochalasin B (H2CB) is a cell division inhibitor that prevents cytokinesis, alters cell morphology, disrupts actin structures in Swiss 3T3 mouse fibroblasts, and inhibits DNA synthesis induced by serum growth factors in quiescent cultures. Low doses of H2CB lead to cell rounding and the loss of actin microfilament bundles.

A 30312 is a fused indole, which overcomes multidrug resistance in P388/Adr cells in vitro. It potentiates the cytotoxicity of the antitumor drugs Adriamycin, vincristine and vinblastine in multidrug-resistant cells with no effect on drug-sensitive parent P388 cells.

FD-211 is a δ lactone originally isolated from M. lutea with anticancer activity.1 It is cytotoxic to adriamycin-susceptible P388, T-24, HeLa, A549, and HL-60 cancer cells (IC50s = 4, 0.5, 1, 1, and 0.2 μg/ml, respectively), as well as adriamycin-resistant HL-60/ADR cells (IC50 = 0.1 μg/ml). FD-211 also inhibits DNA, RNA, and protein synthesis in HeLa cells (IC50 = 1.25 μg/ml for all). |1. Nozawa, O., Okazaki, T., Sakai, N., et al. A novel bioactive δ lactone FD-211. Taxonomy, isolation and characterization. J. Antibiot. (Tokyo) 48(2), 113-118 (1995).