@article {2169, title = {Novel Coumarin-Indole Hybrids as Cytotoxic Candidates: Synthesis and Antiproliferative Activity}, journal = {Pharmacognosy Journal}, volume = {15}, year = {2023}, month = {December 2023}, pages = {1105-1111}, type = {Research Article}, chapter = {1105}, abstract = {

Cancer is regarded as a nightmare for humanity and a challenging task for medical professionals. Twelve hydrides (2a-2l), made of trifunctionalized coumarin and various substituted indoles, were created in an effort to realize the hope of a cancer cure. The 4,5-dimethoxysalicylaldehyde and ethyl acetoacetate were combined in a Knoevenagel reaction to create the coumarin component. The construction of the indole component involved converting various aminoindoles through diazotization and Sandmeyer reactions to twelve substituted indoles (1a-1l). These two components were combined through a Michael addition reaction to create the desired hybrids. Investigating their spectra released from various spectroscopical instruments allowed researchers to determine the 2D molecular frameworks of these hybrids. Studying the survival of nine tumor cell types after treatment with the synthesized hybrids enabled researchers to estimate there in vitro impact as cytotoxic candidates. By checking the cell viability using an MTT marker, it was possible to see that this effect was antiproliferative. The cytotoxicity measurements, IC50 scores, revealed a number of intriguing facts. To start, the synthetic hybrids displayed a relatively similar cytotoxic pattern against the cancerous cell lines under investigation. Second, compared to hybrids with chloride, hydroxyl, or methoxy substituents, fluorinated hybrids are more toxic to cancerous cells. Finally, hybrids with indole substituted at position-6 (2i-2l) have the highest cytotoxicity among those with indole functionalized at position-4 (2a-2d) or position-5 (2e-2h). From these facts, the authors concluded that hybrids with indole substituted at position-4 can represent potential candidates as antiproliferative applicants. Moreover, hybrid 2i may serve as a valuable model for creating potent anti-breast cancer therapies.

}, keywords = {Anti-breast cancer, Coumarin, Cytotoxicity, Indole, Michael addition, MTT}, doi = {10.5530/pj.2023.15.201}, author = {Sarah S. Ismael and Noor Ahmed M. Waheed and Seema Mahmood Kasim and Yasser Fakri Mustafa} } @article {1975, title = {Sub Chronic Toxicity Study of Coumacines}, journal = {Pharmacognosy Journal}, volume = {15}, year = {2023}, month = {March 2023}, pages = {160-164}, type = {Research Article}, chapter = {160}, abstract = {

Coumacine is a brand-new heterocyclic molecular nucleus that was discovered in 2018. In addition to the unique heterocycle known as coumacine, the designer has developed two variants known as coumacine I and II. Coumacine derivatives had been evaluated for their antibacterial effects in vitro against a variety of aerobic and anaerobic bacteria using conventional bacterial strains, using ciprofloxacin and metronidazole as positive controls. The purpose of this research is to look into the relationship between the anticoagulant activity and hepatotoxicity of coumarin and coumacine because the former is a synthetic precursor of the latter and many natural and synthetic coumarins involving warfarin have anticoagulant activity. Thirty male mice were used in this study and exposed to a subchronic dose of 250 or 500 mg/kg of coumacine I or coumacine II. The results of histochemistry showed dramatic changes in hepatocellular morphology that were dose-dependent for both coumacine I and II. Traditionally, higher doses of Coumacine I and II resulted in a significant increase in liver enzymes. Coumacine I or II did no effect on bleeding time. In conclusion, coumacines at subchronic high doses might have hepatotoxic effects through a mechanism that does not affect the coagulation process

}, keywords = {Bleeding, Clotting., Coumacine, Hepatotoxicity}, doi = {10.5530/pj.2023.15.23}, author = {Wejdan Al-Shakarchi and Yasir Saber and Marwan M. Merkhan and Yasser Fakri Mustafa} }