Systematic Review - Chemistry & Clinical Importance of Anticancer Drugs, Plus Recent Advances in Discovery

Abstract

Cancer is a process of uncontrolled cell proliferation that leads to the development of an abnormally growing tumor, determining initially a local disease that might spread, impairing other organs or important processes.One of the most fatal diseases in recent times, cancer kills many lives each year.The effective management of this condition has been impacted by the variances in the disease across the globe, the impact of the medical facilities that are available, and other socioeconomic issues.The aim of this study was to summaries previously published articles regarding recent advances in anticancer drug discoveries.In this review, previously published literature regarding recent advances in anticancer drug discovery collected from journals through Pub Med Central, Google Scholar, and Science Direct from March 20 toMay 12 was identified well, and points that I assumed were important and recent (2017–2023) were included.Anticancer pharmacotherapy has evolved from broadly cytotoxic agents to precision medicines and biologics.This review summarizes the chemistry and clinical importance of major anticancer drug classes (alkylators, antimetabolites, plant alkaloids, topoisomerase inhibitors, kinase inhibitors, hormonal agents, monoclonal antibodies, antibody–drug conjugates (ADCs), immunotherapies and targeted protein degraders such as PROTACs). We highlight recent discovery advances — ADC design, targeted protein degradation (PROTACs/molecular glues), sophisticated kinase/RTK inhibitors, CAR-T and other cellular therapies, and regulatory trends — and outline remaining chemical and translational challenges.

Introduction

Cancer is a multifactorial disease caused by genetic mutations, environmental pollution, food contaminants, radiation, and viruses. It leads to uncontrolled cell growth and tumor formation, making it one of the world’s deadliest diseases. Globally, cancer causes millions of deaths annually, and its burden is projected to increase by 60% in the next two decades. Despite advancements in medical research, effective cancer management remains challenging due to variations in healthcare quality, socioeconomic conditions, and disease complexity.

The pharmaceutical industry has invested heavily in cancer therapy, producing various anticancer drug classes such as cytotoxic drugs, hormone-based therapies, and immunomodulators. However, traditional chemotherapy suffers from issues like non-specificity, toxicity, and drug resistance. To overcome these, researchers are focusing on new molecular targets, monoclonal antibodies, and antibody-drug conjugates that improve selectivity and reduce side effects.

Modern research increasingly uses Artificial Intelligence (AI) and Computer-Aided Drug Design (CADD) for faster and more efficient drug discovery. AI aids in target identification, molecular screening, drug repurposing, and reaction prediction, helping to design small, selective, and less toxic anticancer molecules. Additionally, nanotechnology offers promising solutions for targeted drug delivery through biocompatible and stable nanoparticles.

Recent advances highlight several key targets and therapies:

• Kinase inhibitors (e.g., imatinib, sorafenib) block enzymes involved in cancer cell growth.

• Tubulin/microtubule inhibitors disrupt cell division by targeting the cytoskeleton.

• Vascular targeting agents (VTAs) and angiogenesis inhibitors (e.g., bevacizumab, ramucirumab) prevent tumor blood vessel formation.

• Monoclonal antibodies offer precise, targeted cancer therapies.

Drug repurposing has emerged as a cost-effective strategy, using existing medications for cancer treatment:

• Antiplatelet drugs like aspirin show potential in breast cancer.

• Anti-inflammatory agents (diclofenac, celecoxib) reduce tumor growth and angiogenesis.

• Antidiabetic drugs such as metformin and thiazolidinediones (TZDs) exhibit anti-tumor effects in several cancers.

Conclusion

The global impact of cancer is extremely negative. Beginningwiththefirstnitrogenmustards,researchersand pharmaceuticalcompaniestriedtheirbesttofind cures.Thelackofselectivity,effectiveness,sideeffects,andmetastaticnatureofthediseases make effective treatment challenging, despite the availabilityofawiderangeoftreatmentoptions asalternatives.Recentadvancesinthefieldof molecularbiologyandadeepercomprehensionofthe molecular pathology of cancer have pushed researchers toconcentrateonthedrugtargetsthatcanaidin the total eradication of the disease. The discovery of anticancer drugs is outlined in this review’s recent highlights. Researchers are now betterabletoidentifyspecifictreatmentswithlowertoxicity and better tolerability thanks to recent advances in drug target and discovery. Numerous drug targets have been found for the treatment of cancer based on a variety of articles written by academics, in order to improve their efficacy and decrease their toxicity. The most effective cancertreatmentfocusesarekinase,microtubulin,vascular targeting, angiogenesis, and monoclonal antibodies. Researcherslookintoalternativeusesofadrugthathas already been approved for one condition for other diseases in addition to its original indication in order to significantly reduce the cost, labor, and research time. Antiplatelet,antidiabetic,anti-inflammatory,antimicrobial, and antipsychotic agents are among the repurposed medications that are mentioned. Apopularmethodforfindingnewclassesofanticanceragentsaswellastheirinventivemodesofactionisthroughthediscoveryofphytochemicals. Quercetin,ginseng,artemisinin,andcurcumin allhavethepotentialtofightcancer.Ontheother hand, natural products are recognized as superior andmore potent chemotherapeutic agents. A significantamountofanticanceractivityisexhibited bynewlydevelopedmechanismsthataredesigning novelheterometalliccomplexeswithmetalcenters andheterocyclicandbis-heterocyclicsubstances like thiazolidin-4-ones, 1,3,4-thiadiazoles, and thiazoles to overcome the toxicity of chemotherapies.

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Copyright

Copyright © 2025 Mrs. Hina A. Momin, Ms. Pratiksha S. Gore, Mahadev B. Mundhe. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.