Do Tuong-Ha, Nguyen Dai-Minh, Truong Van-Dat, Do Thi-Hong-Tuoi, Le Minh-Tri, Pham Thanh-Quan, Thai Khac-Minh, Tran Thanh-Dao
Faculty of Applied Sciences, Ton Duc Thang University, 19 Nguyen Huu Tho St., Tan Phong Ward, Dist. 7, Ho Chi Minh City 700000, Vietnam.
Faculty of Pharmacy, University of Medicine and Pharmacy, Ho Chi Minh City, 41 Dinh Tien Hoang St., Dist. 1, Ho Chi Minh City 700000, Vietnam.
Molecules. 2016 Mar 9;21(3):329. doi: 10.3390/molecules21030329.
Chemically diverse heterocyclic chalcones were prepared and evaluated for cytotoxicity, aiming to push forward potency and selectivity. They were tested against rhabdomyosarcoma (RMS) and noncancerous cell line (LLC-PK1). The influence of heteroaryl patterns on rings A and B was studied. Heterocycle functionalities on both rings, such as phenothiazine, thiophene, furan and pyridine were evaluated. Notably, the introduction of three methoxy groups at positions 3, 4, 5 on ring B appears to be critical for cytotoxicity. The best compound, with potent and selective cytotoxicity (IC50 = 12.51 μM in comparison with the value 10.84 μM of paclitaxel), contains a phenothiazine moiety on ring A and a thiophene heterocycle on ring B. Most of the potential compounds only show weak cytoxicity on the noncancerous cell line LLC-PK1.
制备了化学结构多样的杂环查耳酮，并对其细胞毒性进行了评估，旨在提高其效力和选择性。它们针对横纹肌肉瘤（RMS）和非癌细胞系（LLC-PK1）进行了测试。研究了杂芳基模式对A环和B环的影响。评估了两个环上的杂环官能团，如吩噻嗪、噻吩、呋喃和吡啶。值得注意的是，在B环的3、4、5位引入三个甲氧基似乎对细胞毒性至关重要。最佳化合物具有强效和选择性细胞毒性（IC50 = 12.51 μM，相比之下紫杉醇的值为10.84 μM），在A环上含有吩噻嗪部分，在B环上含有噻吩杂环。大多数潜在化合物对非癌细胞系LLC-PK1仅表现出微弱的细胞毒性。
