The antitumor activity of newly synthesised triazolophthalazines (L-45 analogues) 10–32 was evaluated in human hepatocellular carcinoma (HePG-2), breast cancer (MCF-7), prostate cancer (PC3), and colorectal carcinoma (HCT-116) cells. Compounds 17, 18, 25, and 32 showed potent antitumor activity (IC₅₀, 2.83–13.97 μM), similar to doxorubicin (IC₅₀, 4.17–8.87 μM) and afatinib (IC₅₀, 5.4–11.4 μM). HePG2 was inhibited by compounds 10, 17, 18, 25, 26, and 32 (IC₅₀, 3.06–10.5 μM), similar to doxorubicin (IC₅₀, 4.50 μM) and afatinib (IC₅₀, 5.4 μM). HCT-116 and MCF-7 were susceptible to compounds 10, 17, 18, 25, and 32 (IC₅₀, 2.83–10.36 and 5.69–11.36 μM, respectively), similar to doxorubicin and afatinib (IC₅₀ = 5.23 and 4.17, and 11.4 and 7.1 μM, respectively). Compounds 17, 25, and 32 exerted potent activities against PC3 (IC₅₀, 7.56–12.28 μM) compared with doxorubicin (IC₅₀, 8.87 µM) and afatinib (IC₅₀ 7.7 μM). Compounds 17 and 32 were the strongest PCAF inhibitors (IC₅₀, 5.31 and 10.30 μM, respectively) and compounds 18 and 25 exhibited modest IC₅₀ values (17.09 and 32.96 μM, respectively) compared with bromosporine (IC₅₀, 5.00 μM). Compound 17 was cytotoxic to HePG2 cells (IC₅₀, 3.06 μM), inducing apoptosis in the pre-G phase and arresting the cell cycle in the G2/M phase. Molecular docking for the most active PCAF inhibitors (17 and 32) was performed.

在人肝细胞癌（HePG-2），乳腺癌（MCF-7），前列腺癌（PC3）和结直肠癌（HCT-116）中评估了新合成的三唑酞嗪（L-45类似物）10 – 32的抗肿瘤活性。细胞。化合物17，18，25，和32显示出强效的抗肿瘤活性（IC ₅₀，μM2.83-13.97），类似于多柔比星（IC ₅₀，4.17-8.87μM）和阿法（IC ₅₀，μM5.4-11.4）。的HePG2通过化合物抑制10，17，18，25，26，和32（IC ₅₀，3.06-10.5μM），类似于多柔比星（IC ₅₀，μM4.50）和阿法（IC ₅₀，μM5.4）。HCT-116和MCF-7均对化合物10，17，18，25，和32（IC ₅₀，2.83-10.36和5.69-11.36μM，分别地），类似于阿霉素和阿法（IC ₅₀  = 5.23和4.17，分别为11.4和7.1μM）。化合物17，25和32个施加的对抗PC3（IC有力活动₅₀与阿霉素相比，7.56-12.28μM）（IC ₅₀，8.87μM）和阿法（IC ₅₀7.7μM）。化合物17和32分别为最强PCAF抑制剂（IC ₅₀，5.31和10.30微米，分别地）和化合物18个25表现出适度的IC ₅₀值（17.09和32.96μM，分别地）与bromosporine比较（IC ₅₀，μM5.00）。化合物17对HePG2细胞具有细胞毒性（IC ₅₀为3.06μM），在pre-G期诱导细胞凋亡，并在G2 / M期阻止细胞周期。进行了对最具活性的PCAF抑制剂（17和32）的分子对接。