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. 2022 Dec 7;12(54):34965–34983. doi: 10.1039/d2ra07056a

Three-component synthesis and anticancer evaluation of spiropyrrolidine derivatives 17.

graphic file with name d2ra07056a-u4.jpg
Compound R R1 R2 Yield 17 (%) IC50c (μM)
HCT-116 HeLa
17a H H H 92 83.2 ± 0.42 15.1 ± 0.18
17b Cl H H 88 — 10.7 ± 0.15
17c H Me H 62 9.6 ± 0.14 28.4 ± 0.30
17d H H NO2 54 9.3 ± 0.12 16.7 ± 0.14
17e H Me NO2 46 10.9 ± 0.18 25.5 ± 0.28
17f H Cl H 87 12.0 ± 0.20 34.6 ± 0.17
17g H Br H 82 — —
Doxorubicinb — — — — 2.4 ± 0.10 1.8 ± 0.05
a

Reaction conditions: 4-hydroxyquinoline 14 (1.5 mmol), isatine 15 (1.5 mmol), sarcosine 16 (1.5 mmol), MeOH/H2O (2 : 1, v/v), reflux, 2.5–3.0 h.

b

Standard drug for the study.

c

Compound concentration required to reduce HCT-116 and HeLa cells viability by 50% after 48 h treatment relative to 100% DMSO control as assessed with the MTT assay. Data shown are average ± SD of two independent experiments.