Search research articles

ABOUT JoVE

Overview Leadership Blog JoVE Help Center

AUTHORS

Publishing Process Editorial Board Scope & Policies Peer Review FAQ Submit

LIBRARIANS

Testimonials Subscriptions Access Resources Library Advisory Board FAQ

RESEARCH

JoVE Journal Methods Collections JoVE Encyclopedia of Experiments Archive

EDUCATION

JoVE Core JoVE Business JoVE Science Education JoVE Lab Manual Faculty Resource Center Faculty Site

Terms & Conditions of Use

Search research articles

Related Experiment Videos

Intercalators as anticancer drugs.

M F Braña¹, M Cacho, A Gradillas

¹Departamento de Química Orgánica y Farmaceutica, Facultad de Ciencias Experimentales y de la Salud. Monteprincipe. Boadilla del Monte, 28668-Madrid, Spain.

Current Pharmaceutical Design

|September 20, 2001

Summary

DNA intercalators are key cancer drugs that work by inserting into DNA and inhibiting topoisomerase II. This review highlights recent advances and clinical trials, focusing on naphthalimide compounds.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by

Same author

Strain induced in the condyle by self-tapping screws in the Biomet alloplastic temporomandibular joint: a preliminary experimental study.

International journal of oral and maxillofacial surgery·2015

Same author

Comparative assessment of different reconstructive techniques of distal femur in revision total knee arthroplasty.

Knee surgery, sports traumatology, arthroscopy : official journal of the ESSKA·2015

Same author

Mucosal leishmaniasis mimicking squamous cell carcinoma in a liver transplant recipient.

Transplant infectious disease : an official journal of the Transplantation Society·2015

Same author

Prediction at long-term condyle screw fixation of temporomandibular joint implant: A numerical study.

Journal of cranio-maxillo-facial surgery : official publication of the European Association for Cranio-Maxillo-Facial Surgery·2015

Same author

Kidney transplantation with organs from donors after circulatory death type 3: a prospective multicentric Spanish study (GEODAS 3).

Transplantation proceedings·2015

Same author

Pseudo-dynamic analysis of a cemented hip arthroplasty using a force method based on the Newmark algorithm.

Computer methods in biomechanics and biomedical engineering·2014

Area of Science:

Medicinal Chemistry
Molecular Biology
Oncology

Background:

DNA intercalators are crucial compounds that reversibly bind to the DNA double helix.
Many intercalators are established anticancer drugs for ovarian, breast cancers, and leukemias, with others in clinical trials.
Key structural features include planar polyaromatic systems and basic chains, influencing DNA binding affinity and selectivity.

Purpose of the Study:

To review small organic molecules that bind DNA via intercalation.
To focus on compounds exerting antitumor activity through topoisomerase II inhibition.
To provide an overview of recent findings, emphasizing compounds in clinical trials.

Main Methods:

Literature review of DNA intercalators and their mechanisms of action.

Related Experiment Videos

Analysis of structure-activity relationships for antitumor efficacy.

Focus on compounds demonstrating topoisomerase II inhibition.

Main Results:

Intercalator activity is linked to stabilizing the DNA-intercalator-topoisomerase II ternary complex.
Naphthalimides, developed since the 1970s, are a significant class of intercalators.
Several intercalating agents are progressing through clinical trials for various cancers.

Conclusions:

DNA intercalation remains a vital strategy in cancer chemotherapy.
Topoisomerase II inhibition is a critical mechanism for the antitumor effects of many intercalators.
Ongoing research and clinical trials continue to explore novel intercalating agents, including naphthalimides, for cancer treatment.