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RTI.2013 - Colchicine derivatives as antineoplasic agents: patent filling


Cellular microtubules are anticancer targets extensively validated in the clinic. Anti-tubulin agents that interact with the colchicine binding site are attracting a lot of interest for development of new drugs against cancer. We have designed, synthesized and tested a series of colchicine analogues and assessed their potential as anti-cancer agents. Compounds obtained showed in vitro anti-leukemic effects at the nanomolar concentration range, strongly blocked cell cycle progression in G2/M and induced cell death through apoptosis. a single weekly i.p. dose of 1 mg/kg of one colchicine analogue significantly slowed the progression of primary human Acute Lymphoblastic Leukemia (ALL) in NOD/Scid mice, the effect being comparable to that obtained with vincristine, as evaluated by the enumeration of ALL cells in the peripheral blood, bone marrow, spleen and liver. No toxicity was recorded. Animals treated one month with the colchicine analogue survived significantly longer than control: 69 days versus 36 days, at the higher dose given (0.5mg/kg/3x per week). (AU)

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