Probing structural requirements for thiazole-based mimetics of sunitinib as potent VEGFR-2 inhibitors.

Novel thiazole analogs 3a, 3b, 4, 5, 6a-g, 8a, 8b, 9a-c, 10a-d and 11 were designed and synthesized as molecular mimetics of sunitinib. antitumor activity of the obtained compounds was investigated against HepG2, HCT-116, MCF-7, HeP-2 and HeLa cancer cell lines. The obtained data showed that compounds 3b and 10c are the most potent members toward HepG2, HCT-116, MCF-7 and HeLa cells.

Perfusion-MRI for differentiating cerebral metastatic lesions and gliomas: An evidence-based review.

Background: Lesions affecting the brain are variable and have multiple pathologies. Brain metastasis is a common entity of lesions that can be misleading in diagnosis. Brain metastasis affects the patient's life and survival in about 40% of cases; all patients with metastatic brain lesions are indicated for surgery, so proper diagnosis is crucial for each patient.

Small-cell neuroendocrine carcinoma of the cervix with leptomeningeal spread: A rare coincidence report and literature review.

Background: Metastasis from cancers of the cervix to the central nervous system is relatively uncommon. Small-cell neuroendocrine cancer of the cervix is a very rare tumor with a high tendency to spread early.

Case Description: A 33-year-old-woman was diagnosed with a small-cell neuroendocrine cancer of the cervix after complaining about a long time of post-coital bleeding.

Design, synthesis, and antitumor screening of new thiazole, thiazolopyrimidine, and thiazolotriazine derivatives as potent inhibitors of VEGFR-2.

New thiazole, thiazolopyrimidine, and thiazolotriazine derivatives 3-12 and 14a-f were synthesized. The newly synthesized analogs were tested for in vitro antitumor activity against HepG2, HCT-116, MCF-7, HeP-2, and Hela cancer cells. Results indicated that compound 5 displayed the highest potency toward the tested cancer cells.

Design, synthesis, and evaluation of new benzimidazole‏ ‏‎thiourea ‎derivatives as antitumor agents.

Novel benzimidazole thiourea derivatives were designed and synthesized based on sorafenib as a lead compound. The benzimidazole moiety was traded by the pyridine ring to enhance the hydrophobic interaction and retain hydrogen bonding in the hinge region, while lipophilic moieties with different bulkiness were employed in the deep hydrophobic pocket for better hydrophobic interactions. Thiourea as a urea bioisostere was also utilized.