Series of diethyl 2,5-diaminothiophene-3,4-dicarboxylate (DDTD) derivatives: azomethines of DDTD (2a–l) have been synthesized and screened for their anticancer, antimicrobial and anti-diabetic activities. The novel synthesized compounds were characterized by ¹H, ¹³C NMR, MS and FT-IR analyses. All compounds were evaluated for their antiproliferative activity against three types of cancer cell line such as T47D and MCF-7 (human breast cancer), Hela (human cervical cancer) and Ishikawa (human endometrial cancer) lines. The results showed that most compounds exhibited significant antiproliferative activity against breast cancer cells. The majority of azomethines DDTD influenced strongly against breast cancer cells T47D and MCF-7, among them compounds 2b (2.3 μM), 2c (12.1 μM), 2e (13.2 μM), 2i (14.9 μM), 2j (16.0 μM), 2k (7.1 μM), 2l (8.6 μM) manifest potent anticancer activity against cancer cell T47D than Doxorubicin (DOX, 15.5 μM). Compound 2j has shown potent activity on all three types of cancer cells concurrently and IC₅₀ values were considerably low in comparison with positive control DOX. In addition, all compounds were tested for antimicrobial activity against Staphylococcus aureus ATCC 6538 (Gram positive bacteria), Escherichia coli ATCC 11229 (Gram negative bacteria) and Candida albicans ATCC 10231 (Fungi) strains and 2j which contains in the ring nitrofurfural fragment, showed the highest effect on the three species of microbial pathogens simultaneously. Some compounds induced enzymatic inhibition in a concentration-dependent manner on PTP-1B inhibitor.

2，5-二氨基噻吩-3，4-二羧酸二乙酯（DDTD）衍生物系列：DDTD的甲亚胺（2a - 1）已经合成并筛选出其抗癌，抗微生物和抗糖尿病活性。新型合成化合物的特征在于¹ H，¹³13 C NMR，MS和FT-IR分析。评估了所有化合物对三种类型的癌细胞系（例如T47D和MCF-7（人类乳腺癌），Hela（人类宫颈癌）和Ishikawa（人类子宫内膜癌））的抗增殖活性。结果表明，大多数化合物对乳腺癌细胞显示出显着的抗增殖活性。大多数偶氮甲碱DDTD对乳腺癌细胞T47D和MCF-7有强烈影响，其中化合物2b（2.3μM），2c（12.1μM），2e（13.2μM），2i（14.9μM），2j（16.0μM），2k（7.1μM），2公升（8.6μM）比阿霉素（DOX，15.5μM）表现出对癌细胞T47D的有效抗癌活性。化合物2j已同时显示出对所有三种类型癌细胞的有效活性，与阳性对照DOX相比，IC ₅₀值相当低。此外，测试了所有化合物对金黄色葡萄球菌ATCC 6538（革兰氏阳性细菌），大肠杆菌ATCC 11229（革兰氏阴性细菌）和白色念珠菌ATCC 10231（真菌）菌株和2j的抗菌活性。环中的糠醛碎片中含有的三聚氰胺同时对三种微生物病原体表现出最高的作用。一些化合物以浓度依赖的方式诱导对PTP-1B抑制剂的酶促抑制作用。