# Anticancer potential of fused heterocycles: structural insights and mechanistic advances

**Authors:** Aaysha Pandey, Shubham Sharma, Kamal Kishore, Swati Rani, Man Vir Singh, Gangotri Pemawat

PMC · DOI: 10.2478/abm-2025-0035 · Asian Biomedicine: Research, Reviews and News · 2025-12-31

## TL;DR

This paper reviews how certain fused heterocycle compounds show strong anticancer potential through multiple biological mechanisms.

## Contribution

The paper provides a comprehensive review of the anticancer efficacy and mechanisms of specific fused heterocycle compounds.

## Key findings

- Fused heterocycles show significant anticancer activity in multiple cell lines with low IC50 values.
- These compounds act through DNA interaction, kinase inhibition, microtubule disruption, and enzyme inhibition.
- They are promising candidates for targeted and multi-mechanistic cancer therapy.

## Abstract

β-lactam derivatives, carbazoles, isatin derivatives, pyrrolo-benzodiazepines (PBDs), and pyrido[2,3-d]pyrimidines have demonstrated potential as anticancer agents among organic compounds. They exhibit substantial anticancer efficacy across several cancer cell lines, such as HL-60, THP-1, U-937, HeLa, PANC1, MDA-MB-231, and A549 cell lines. These compounds display a significant anticancer profile via diverse biological pathways such as DNA interaction, kinase inhibition, microtubule disruption, and enzyme inhibition. Their low IC50 values across various cell lines suggest their viability as strong candidates for targeted and multi-mechanistic cancer therapy, warranting further in vivo and clinical exploration. This review thoroughly summarized the anticancer efficacy of β-lactam derivatives, carbazoles, isatins, PBDs, and pyrido[2,3-d]pyrimidine derivatives.

## Full-text entities

- **Genes:** MAOB (monoamine oxidase B) [NCBI Gene 4129], BCL2 (BCL2 apoptosis regulator) [NCBI Gene 596] {aka Bcl-2, PPP1R50}, RIEG2 (Rieger syndrome 2) [NCBI Gene 6012] {aka ARS, RGS2}, IKBKB (inhibitor of nuclear factor kappa B kinase subunit beta) [NCBI Gene 3551] {aka IKK-2, IKK-beta, IKK2, IKKB, IMD15, IMD15A}, TNF (tumor necrosis factor) [NCBI Gene 7124] {aka DIF, IMD127, TNF-alpha, TNFA, TNFSF2, TNLG1F}, PLG (plasminogen) [NCBI Gene 5340] {aka HAE4}, DHFR (dihydrofolate reductase) [NCBI Gene 1719] {aka DHFR1, DYR}, HPSE (heparanase) [NCBI Gene 10855] {aka HPA, HPA1, HPR1, HPSE1, HSE1}, NFKB1 (nuclear factor kappa B subunit 1) [NCBI Gene 4790] {aka CVID12, EBP-1, KBF1, NF-kB, NF-kB1, NF-kappa-B1}
- **Diseases:** cytotoxic (MESH:D064420), bone marrow suppression (MESH:D001855), plasma tumor (MESH:D010954), colorectal cancer (MESH:D015179), leukemia (MESH:D007938), breast cance (MESH:D061325), deaths (MESH:D003643), hypertension (MESH:D006973), fungal infections (MESH:D009181), hepatitis (MESH:D056486), T-cell leukemia (MESH:D015458), breast cancer (MESH:D001943), bacterial infections (MESH:D001424), promyelocytic leukemia (MESH:D015473), anxiety (MESH:D001007), Cancer (MESH:D009369), lung cancer (MESH:D008175), acute monocytic leukemia (MESH:D007948), prostate cancer (MESH:D011471), inflammation (MESH:D007249), carcinogenic diseases (MESH:D004194), emesis (MESH:D014839), human papillomavirus infections (MESH:D030361), diarrhea (MESH:D003967), Burkitt's lymphoma (MESH:D002051), vertigo (MESH:D014717), skin cancer (MESH:D012878), stomach cancer (MESH:D013274)
- **Chemicals:** Nocodazole (MESH:D015739), nicotine (MESH:D009538), Anthramycin (MESH:D000876), sibiromycin (MESH:C100298), o-phenylenediamine (MESH:C034193), Etoposide (MESH:D005047), MTT (MESH:C070243), Carbazoles (MESH:D002227), thiamine (MESH:D013831), gefitinib (MESH:D000077156), cephalosporin (MESH:D002511), tomaymycin (MESH:C003619), abbeymycin (MESH:C052313), caffeine (MESH:D002110), PBD (MESH:C438462), penicillin (MESH:D010406), benzodiazepine (MESH:D001569), pyridine (MESH:C023666), Doxorubicin (MESH:D004317), 3-(4,5-dimethyl thiazole-2-yl)-2,5-diphenyl tetrazolium bromide (MESH:C022616), S (MESH:D013455), 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium (-), folate (MESH:D005492), DHA (MESH:C027493), indole (MESH:C030374), nintedanib (MESH:C530716), tryptophan (MESH:D014364), morphine (MESH:D009020), beta-Lactam (MESH:D047090), oxindole (MESH:C022960), semaxinib (MESH:C116890), Ribociclib (MESH:C000589651), purine (MESH:C030985), pyrrole (MESH:D011758), diazomethane (MESH:D003978), Toceranib phosphate (MESH:C464577), morpholine (MESH:C037574), ATP (MESH:D000255), triazole (MESH:D014230), adrenaline (MESH:D004837), Ellipticine (MESH:C034192), beta-Lactam antibiotics (MESH:D008997), carbon (MESH:D002244), ketones (MESH:D007659), indolinone (MESH:D000078183), lactam (MESH:D007769), azide (MESH:D001386), N (MESH:D009584), celiptium (MESH:C027767), sulfonamides (MESH:D013449), isoxazole (MESH:D007555), Taxol (MESH:D017239), Carbazole (MESH:C041514), orantinib (MESH:C412603), mazethramycin (MESH:C027073), O (MESH:D010100), zinc (MESH:D015032), pyrimidine (MESH:C030986), aldehyde (MESH:D000447), chicamycin A (MESH:C041408)
- **Species:** Homo sapiens (human, species) [taxon 9606], Couroupita guianensis (cannonball tree, species) [taxon 66684], Ochrosia elliptica (species) [taxon 141591], Isatis tinctoria (woad, species) [taxon 161756], Penicillium (genus) [taxon 5073], Streptomyces refuineus (species) [taxon 223296], Melochia tomentosa (species) [taxon 1127084]
- **Cell lines:** T-47D — Homo sapiens (Human), Invasive breast carcinoma of no special type, Cancer cell line (CVCL_0553), A431 — Homo sapiens (Human), Skin squamous cell carcinoma, Cancer cell line (CVCL_0037), SK-BR-3 — Homo sapiens (Human), Breast adenocarcinoma, Cancer cell line (CVCL_0033), THP-1 — Homo sapiens (Human), Childhood acute monocytic leukemia, Cancer cell line (CVCL_0006), Jurkat — Homo sapiens (Human), Childhood T acute lymphoblastic leukemia, Cancer cell line (CVCL_0065), MDA-MB-436 — Homo sapiens (Human), Invasive breast carcinoma of no special type, Cancer cell line (CVCL_0623), MDA MB-231 — Homo sapiens (Human), Breast adenocarcinoma, Cancer cell line (CVCL_0062), HeLa — Homo sapiens (Human), Human papillomavirus-related endocervical adenocarcinoma, Cancer cell line (CVCL_0030), HT-29 — Homo sapiens (Human), Colon adenocarcinoma, Cancer cell line (CVCL_0320), A375 — Homo sapiens (Human), Amelanotic melanoma, Cancer cell line (CVCL_0132), BT-474 — Homo sapiens (Human), Invasive breast carcinoma of no special type, Cancer cell line (CVCL_0179), PANC-1 — Homo sapiens (Human), Pancreatic ductal adenocarcinoma, Cancer cell line (CVCL_0480), Colo205 — Homo sapiens (Human), Colon adenocarcinoma, Cancer cell line (CVCL_0218), PC-3 — Homo sapiens (Human), Prostate carcinoma, Cancer cell line (CVCL_0035), A-549 — Homo sapiens (Human), Lung adenocarcinoma, Cancer cell line (CVCL_0023), Jurkat leukemia — Homo sapiens (Human), Childhood B acute lymphoblastic leukemia, Cancer cell line (CVCL_6G43), HL-60 — Homo sapiens (Human), Adult acute myeloid leukemia with maturation, Cancer cell line (CVCL_0002), HepG-2 — Homo sapiens (Human), Hepatoblastoma, Cancer cell line (CVCL_0027), U-937 — Homo sapiens (Human), Adult acute monocytic leukemia, Cancer cell line (CVCL_0007), MCF-7 — Homo sapiens (Human), Invasive breast carcinoma of no special type, Cancer cell line (CVCL_0031), HCT-116 — Homo sapiens (Human), Colon carcinoma, Cancer cell line (CVCL_0291), B16F10 — Mus musculus (Mouse), Mouse melanoma, Cancer cell line (CVCL_0159)

## Full text

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## Figures

13 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12919380/full.md

## References

95 references — full list in the complete paper: https://tomesphere.com/paper/PMC12919380/full.md

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Source: https://tomesphere.com/paper/PMC12919380