Indole-thiazole hybrids with anticancer potential

Lianlian Chen1, Danchen Zhao1, Kesong Zhu1

  • 1School of Pharmacy, Xianning Medical College, Hubei University of Science and Technology, Xianning, Hubei, China.

PubMed

Insights

Novel indole-thiazole hybrids show enhanced anticancer activity and selectivity. This review details their structure-activity relationships and mechanisms, paving the way for improved cancer drug design.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Drug Discovery

Background:

  • Traditional chemotherapeutics face limitations including drug resistance, poor selectivity, and toxicity.
  • Indole and thiazole scaffolds are recognized for their anticancer properties and favorable pharmacokinetic profiles.
  • Hybridizing these scaffolds offers a synergistic approach to developing more effective anticancer agents.

Purpose of the Study:

  • To review recent advancements (since 2021) in the anticancer potential of indole-thiazole hybrids.
  • To analyze structure-activity relationships (SARs) governing the potency of these hybrids.
  • To explore their mechanisms of action and interactions with biomolecular targets.

Main Methods:

  • Systematic literature review of indole-thiazole hybrids developed post-2021.
  • Detailed structure-activity relationship (SAR) analysis.
  • Exploration of molecular targets and signaling pathways modulated by these hybrids.

Main Results:

  • Indole-thiazole hybrids demonstrate enhanced antiproliferative efficacy against cancer cells.
  • These hybrids exhibit improved target selectivity and reduced toxicity to normal cells compared to individual components.
  • Key molecular features contributing to anticancer potency have been identified through SAR analysis.

Conclusions:

  • Indole-thiazole hybrids represent a promising class of anticancer agents with superior efficacy and safety profiles.
  • Understanding their SARs and mechanisms of action is crucial for rational drug design.
  • This review provides a foundation for developing next-generation indole-thiazole-based cancer therapeutics.

Related Concept Videos

Hybrid Zones02:29

Hybrid Zones

Hybrid zones are narrow regions where two closely related species interact, mate, and produce hybrids. Relative to either parent species, hybrids may possess distinct phenotypic or genetic differences that impact their survival and reproductive success. The genetic variances introduced by hybridization influence species diversity and speciation processes within the hybrid zone.
21.9K
Hybridization of Atomic Orbitals I03:24

Hybridization of Atomic Orbitals I

The mathematical expression known as the wave function, ψ, contains information about each orbital and the wavelike properties of electrons in an isolated atom. When atoms are bound together in a molecule, the wave functions combine to produce new mathematical descriptions that have different shapes. This process of combining the wave functions for atomic orbitals is called hybridization and is mathematically accomplished by the linear combination of atomic orbitals. The new orbitals that...
67.2K
Hybridization of Atomic Orbitals II03:35

Hybridization of Atomic Orbitals II

sp3d and sp3d 2 Hybridization
49.0K
Potential Energy00:52

Potential Energy

The energy stored by a structure and location of matter in space is called potential energy. For instance, raising a kettlebell changes its spatial location and increases its potential energy. Similarly, a stretched rubber band contains potential energy which, under certain conditions, can be converted into other forms of energy, such as kinetic energy.
Chemical bonds that form attractive forces between atoms also contain potential energy, called chemical energy. When a chemical reaction...
42.7K
Potential Energy01:09

Potential Energy

A conservative force, such as a gravitational or elastic force, gives the body the capacity to do work. This capacity, measured as the potential energy, depends on the body's location or “position” relative to a fixed reference position or datum. The gravitational potential energy is considered zero at the reference point. Suppose a body is located at some vertical distance above a fixed horizontal reference or datum. In that case, the weight of the body has positive gravitational potential...
999
Standard Electrode Potentials03:02

Standard Electrode Potentials

On comparing the reactivity of silver and lead, it is observed that the two ionic species, Ag+ (aq) and Pb2+ (aq), show a difference in their redox reactivity towards copper: the silver ion undergoes spontaneous reduction, while the lead ion does not. This relative redox activity can be easily quantified in electrochemical cells by a property called cell potential. This property is commonly known as cell voltage in electrochemistry, and it is a measure of the energy which accompanies the charge...
50.3K