Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs. The compounds and compositions can be used to treat and / or prevent a wide variety of cancers, including 
drug resistant cancers. While the antitussive 
plant alkaloid, noscapine, binds 
tubulin, displays anticancer activity, and has a safe pharmacological profile in humans, structure-function analyses pointed to a 
proton at position 9 of the 
isoquinoline ring that can be modified without compromising 
tubulin binding activity. Noscapine analogs with various functional moieties at position 9 on the 
isoquinoline ring kill 
human cancer cells resistant to other anti-
microtubule agents, such as vincas and taxanes. Representative analogs include the 9-nitro, 9-bromo-, 9-iodo-, and 9-fluoro-noscapines, which bind 
tubulin and induce 
apoptosis selectively in 
tumor cells (ovarian and T-
cell lymphoma) resistant to 
paclitaxel, 
vinblastine and 
teniposide. Surprisingly, treatment with one of the analogs, 9-nitro-nos, at doses as high as 100 μM, did not affect the 
cell cycle profile of normal human fibroblasts. This selectivity for 
cancer cells represents a unique edge over the other available antimitotics. The compounds can perturb the progression of 
cell cycle by mitotic arrest, followed by 
apoptotic cell death associated with increased 
caspase-3 activation and appearance of TUNEL-positive cells. Thus, the compounds are novel therapeutic agents for a variety of cancers, including ovarian and T-
cell lymphoma cancers, even those that have become 
drug-resistant to currently available 
chemotherapeutic drugs.