New azafluorenones, 2-aryl-4-(4-hydroxyphenyl)-5H-indeno[1,2-b]pyridin-5-ones, were prepared to evaluate their cytotoxic/anticancer properties, also their inhibitory effects on hCA I and II isoenzymes. Aryl part was changed as [phenyl (H1), 4-methylphenyl (H2), 4-methoxyphenyl (H3), 4-fluorophenyl (H4), 4-bromophenyl (H5), 4-chlorophenyl (H6), 3-hydroxyphenyl (H7), and 4-hydroxyphenyl (H8)]. The structure of the synthesized compounds was characterized by ¹H NMR, ¹³C NMR and HRMS spectra.

Cytotoxicity results of the series pointed out that the compounds H6 (PSE: 28.0) and H5 (PSE: 27.3), with the highest potency selectivity expression (PSE) value, can be considered as leader compounds of the study in designing novel anticancer agents. Additionally, all azafluorenones synthesized showed a good inhibition profile towards hCA I and II isoenzymes in the range of 54.14–73.72 nM and 67.28–76.15 nM, respectively.

The compounds H5 and H6 can be considered for further designs with their cytotoxic and CA inhibitory profiles.

制备了新的氮杂芴酮2-芳基-4-（4-羟苯基）-5 H-茚并[1,2 - b ]吡啶基-5-酮，以评估其细胞毒性/抗癌特性，以及它们对hCA I和HCA I的抑制作用。 II同工酶。芳基部分更改为[苯基（H1），4-甲基苯基（H2），4-甲氧基苯基（H3），4-氟苯基（H4），4-溴苯基（H5），4-氯苯基（H6），3-羟基苯基（H7）和4-羟基苯基（H8）]。合成的化合物的结构通过¹ H NMR，¹³ C NMR和HRMS光谱表征。

该系列的细胞毒性结果指出，具有最高效能选择性表达（PSE）值的化合物H6（PSE：28.0）和H5（PSE：27.3），可以被认为是设计新型抗癌药物的主要研究化合物。此外，所有合成的氮杂芴酮对hCA I和II同工酶均表现出良好的抑制特性，分别在54.14-73.72 nM和67.28-76.15 nM之间。

化合物H5和H6具有细胞毒性和CA抑制特性，可以考虑用于进一步设计。