Melanoma is the most serious type of skin cancer. It is the 5-7th most common cancer in the United States and the incidence of this cancer is increasing rapidly. Other than the skin, this cancer can also develop in eyes and in internal organs such as intestines. The risk of melanoma is higher in people under 40, especially in Caucasian women.  In 2011, about 9,000 Americans died from this disease and the number is expected to rise up to 10,130 in 2016. In 2011, melanoma incidence and death rates were 19.7 and 2.7 per 100,000, respectively. The cost of treating of newly diagnosed melanomas will increase from $457 million in 2011 to $1.6 billion in 2030. Additional efforts are required to prevent the incidence, death, and health care cost of this disease. Development of new therapeutic options is urgently needed to treat this rapidly rising malignancy. Pyrazole is a two nitrogen-containing heterocycle. N-phenyl and 1,2-diphenyl pyrazole derivatives are privileged structures in drug development. Many pyrazole-derived drugs are among the best-selling medicines. They are pharmaceutically attractive because of their high potency, metal chelation property, specificity towards enzymes, broad spectrum of bioactivity, solubility, stability, and low toxicity. Antitumor activities of pyrazole derivatives are known to result from their inhibitory activities against BRAF<sup>V600E</sup>, EGFR, telomerase, ROS receptor tyrosine kinase, and many other kinases. Crizotinib, a pyrazole derivative, is an ALK (anaplastic lymphoma kinase) and ROS1 (c-ros oncogene 1) inhibitor and it has been approved to treat non-small cell lung cancer. We have found several pyrazole and fused thiazoline-androstanedione based novel molecules as potent cytotoxic agents several melanoma cell lines. In this presentation, we will present the synthesis and cytotoxic studies of several novel molecules against several melanoma cell lines.<br/>

Antimelanoma studies of novel pyrazole and fused thiazoline-androstanedione derivatives

255th National Meeting (2018)

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