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Siddiqui et al. Chem Synth 2023;3:25 https://dx.doi.org/10.20517/cs.2023.02 Page 35 of 50

Figure 59. Microbial transformation of exemestane (318) with Cunninghamella blakesleeana.

Figure 60. Microbial transformation of exemestane (318) with Curvularia lunata, Gibberella fujikuroi, and Aspergillus niger.

(4.2%), and 2α-methyl-5α-androsta-17β-hydroxy-3-one (342) (0.5%) were produced by the
biotransformation of the anti-cancer drug, drostanolone enanthate (334), with Cephalosporium aphidicola
[81]
and Fusarium lini [Figure 61].

Metabolite 341 (IC = 19.6 ± 1.4 µM) exhibited potent activity against HeLa (cervical) cancer cells, in
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contrast to the parent drug 334 (IC = 54.7 ± 1.6 µM), and the standard drug, cisplatin (IC = 40.1 ± 2.0 µ
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M). Compounds 335 (IC = 64.3 ± 3.0 µM), 336 (IC = 40.7 ± 0.9 µM), 337 (IC = 40.7 ± 0.9 µM), 338 (IC =
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49.5 ± 2.2 µM), 339 (IC = 39.8 ± 1.5 µM), and 342 (IC = 30.1 ± 1.0 µM) also displayed remarkable activity
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against HeLa cell line. Metabolites 335 (IC = 58.4 ± 1.6 µM), 336 (IC = 59.1 ± 2.6 µM), 337 (IC = 60.4 ±
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0.9 µM), 338 (IC = 51.8 ± 3.4 µM), 339 (IC = 68.1 ± 1.2 µM), and 340 (IC = 39.1 ± 2.0 µM) showed a
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significant anti-cancer activity against PC-3 (prostate) cells, compared to compounds 342 (IC = 96.2 ± 3.0 µ
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M), 335 (IC = 84.6 ± 6.4 µM), 339 (IC = 84.0 ± 3.1 µM), and standard cisplatin (IC = 76.5 ± 1.2 µM).
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Compounds 334 (IC = 5.0 ± 1.2 µM), 338 (IC = 12.4 ± 2.3 µM), 340 (IC = 16.7 ± 2.6 µM), and
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