Rho GTPase B (RhoB), a member of RhoA-like isoforms is a family of Ras-homologous GTPase which is considered as a potent target of anticancer therapy. Modulating RhoB is an important role for inhibiting certain tumor survival pathways, because only one isoform, RhoB is related in tumor suppression, whereas other Rho isoforms are related in tumor proliferation. Even though RhoB can be a good target for anticancer therapy, only few chemical entities are used for regulating RhoB protein. G02, found as a good lead compound, has good anti-proliferative activity for NUGC-3 cell lines. Based on the structure of G02, we designed and synthesized numerous derivatives which have a good tumor inhibitory activity. Among these analogs, A665 has been selected as a potent candidate for anticancer therapy, especially in PC-3 and NUGC-3 cell lines. Even though the acute binding mechanism between RhoB protein and our derivatives is not clear yet, experimental data and biological evaluation of derivatives showed that A665 could be an excellent candidate for anti-cancer therapy.

Design, synthesis, and evaluation of novel RhoB modulating agents for anticancer chemotherapy

239th National Meeting (2010)

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